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Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.

ABSTRACT: A new series of phenylthiazoles with t-butyl lipophilic component was synthesized and their antibacterial activity against a panel of multidrug-resistant bacterial pathogens was evaluated. Five compounds demonstrated promising antibacterial activity against methicillin-resistant staphylococcal strains and several vancomycin-resistant staphylococcal and enterococcal species. Additionally, three derivatives 19, 23 and 26 exhibited rapid bactericidal activity, and remarkable ability to disrupt mature biofilm produced by MRSA USA300. More importantly, a resistant mutant to 19 couldn't be isolated after subjecting MRSA to sub-lethal doses for 14 days. Lastly, this new series of phenylthiazoles possesses an advantageous attribute over the first-generation compounds in their stability to hepatic metabolism, with a biological half-life of more than 9?h.

SUBMITTER: Kotb A

PROVIDER: S-EPMC5924651 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature

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Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.

Kotb Ahmed A Abutaleb Nader S NS Seleem Mohamed A MA Hagras Mohamed M Mohammad Haroon H Bayoumi Ashraf A Ghiaty Adel A Seleem Mohamed N MN Mayhoub Abdelrahman S AS

European journal of medicinal chemistry 20180319

A new series of phenylthiazoles with t-butyl lipophilic component was synthesized and their antibacterial activity against a panel of multidrug-resistant bacterial pathogens was evaluated. Five compounds demonstrated promising antibacterial activity against methicillin-resistant staphylococcal strains and several vancomycin-resistant staphylococcal and enterococcal species. Additionally, three derivatives 19, 23 and 26 exhibited rapid bactericidal activity, and remarkable ability to disrupt matu ...[more]

PMID: 29605807

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